[HTML][HTML] The importance of cellular degradation kinetics for understanding mechanisms in targeted protein degradation
Targeted protein degradation has exploded over the past several years due to preclinical
and early clinical therapeutic success of numerous compounds, and the emergence of new …
and early clinical therapeutic success of numerous compounds, and the emergence of new …
Cellular resistance mechanisms to targeted protein degradation converge toward impairment of the engaged ubiquitin transfer pathway
P Ottis, C Palladino, P Thienger, A Britschgi… - ACS chemical …, 2019 - ACS Publications
Proteolysis targeting chimeras are bifunctional small molecules capable of recruiting a target
protein of interest to an E3 ubiquitin ligase that facilitates target ubiquitination followed by …
protein of interest to an E3 ubiquitin ligase that facilitates target ubiquitination followed by …
Structural basis for the selection of glycosylated substrates by SCFFbs1 ubiquitin ligase
T Mizushima, Y Yoshida… - Proceedings of the …, 2007 - National Acad Sciences
The ubiquitin ligase complex SCFFbs1, which contributes to the ubiquitination of
glycoproteins, is involved in the endoplasmic reticulum-associated degradation pathway. In …
glycoproteins, is involved in the endoplasmic reticulum-associated degradation pathway. In …
The Prp19 U-box Crystal Structure Suggests a Common Dimeric Architecture for a Class of Oligomeric E3 Ubiquitin Ligases,
CW Vander Kooi, MD Ohi, JA Rosenberg… - Biochemistry, 2006 - ACS Publications
Prp19 is an essential splicing factor and a member of the U-box family of E3 ubiquitin
ligases. Prp19 forms a tetramer via a central coiled-coil domain. Here, we show the U-box …
ligases. Prp19 forms a tetramer via a central coiled-coil domain. Here, we show the U-box …
[HTML][HTML] pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4CRBN ubiquitin ligase
Thalidomide and its derivatives lenalidomide and pomalidomide (IMiDs) are effective
treatments of haematologic malignancies. It was shown that IMiDs impart gain-of-function …
treatments of haematologic malignancies. It was shown that IMiDs impart gain-of-function …
[HTML][HTML] Plasticity of the Cullin-RING ligase repertoire shapes sensitivity to ligand-induced protein degradation
Inducing protein degradation via small molecules is a transformative therapeutic paradigm.
Although structural requirements of target degradation are emerging, mechanisms …
Although structural requirements of target degradation are emerging, mechanisms …
Recognition of substrate degrons by E3 ubiquitin ligases and modulation by small-molecule mimicry strategies
Highlights•E3 ligases recruit substrates for proteasomal degradation by recognition of
degrons.•Crystal structures reveal the structural basis and mechanism of degron …
degrons.•Crystal structures reveal the structural basis and mechanism of degron …
[HTML][HTML] SCFFbxo22-KDM4A targets methylated p53 for degradation and regulates senescence
Y Johmura, J Sun, K Kitagawa, K Nakanishi… - Nature …, 2016 - nature.com
Recent evidence has revealed that senescence induction requires fine-tuned activation of
p53, however, mechanisms underlying the regulation of p53 activity during senescence …
p53, however, mechanisms underlying the regulation of p53 activity during senescence …
E3 ubiquitin ligase that recognizes sugar chains
Y Yoshida, T Chiba, F Tokunaga, H Kawasaki, K Iwai… - Nature, 2002 - nature.com
N-glycosylation of proteins in the endoplasmic reticulum (ER) has a central role in protein
quality control,,. Here we report that N-glycan serves as a signal for degradation by the Skp1 …
quality control,,. Here we report that N-glycan serves as a signal for degradation by the Skp1 …
Targeting Cullin–RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation
In the last decade, the ubiquitin–proteasome system has emerged as a valid target for the
development of novel therapeutics. E3 ubiquitin ligases are particularly attractive targets …
development of novel therapeutics. E3 ubiquitin ligases are particularly attractive targets …